The antitumor activity of PNA modified vinblastine cationic liposomes on Lewis lung tumor cells: In vitro and in vivo evaluation

Non-small cell lung cancer (NSCLC) is one of the frequently-occurring disease in the world, and the treatment effects are usually unsatisfactory. Vinblastine is an anti-microtubule drug in clinic. In this study, a nanostructured liposome was designed and prepared for treating NSCLC. In the liposomes, peanut agglutinin (PNA) was modified on the liposomal surface, 3-(N-(N',N'-dimethylaminoethane) carbamoyl) cholesterol was used as cationic materials, and vinblastine was encapsulated in the aqueous core of liposomes, respectively. The PNA modified vinblastine cationic liposomes were approximately 100 nm in size with a positive potential. In vitro results showed that the targeting liposomes could significantly enhance cellular uptake, selectively accumulate in LLT cells, and dramatically initiate apoptosis via activating pro-apoptotic proteins and apoptotic enzymes, thus leading to the strongest antitumor efficacy to LLT cells. In vivo results demonstrated that the targeting liposomes could display a prolonged circulation time in the blood, accumulate more drug in tumor location, and induce most of tumor cells apoptosis. As a result, a robust overall antitumor efficacy in tumor-bearing mice was observed subsequently. In conclusion, the chemotherapy using the PNA modified vinblastine cationic liposomes could provide a potential strategy for treating non-small cell lung cancer. (C) 2015 Elsevier B.V. All rights reserved.